Norfloxacin, pills 400mg 10pcs

Composition

of film-coated tablets.

film-coated tablets.

for 1 tablet:

Norfloxacin – 400 mg

Excipients

[colloidal silicon dioxide (aerosil) – 7.2 mg

magnesium stearate-7.2 mg

microcrystalline cellulose-240.8 mg

croscarmellose sodium-21.6 mg

crospovidone] – 43.2 mg

The average weight of a tablet without a shell is 720 mg

Excipients for the shell

hypromellose (hydroxypropylmethylcellulose) -13.14 mg

macrogol 6000 (polyethylene glycol 6000) – 4.4 mg

titanium dioxide-4.4 mg

quinoline yellow dye-0.06 mg

Pharmacological action

Pharmaceutical group:

antimicrobial agent-fluoroquinolone. Pharmacodynamics :

Antimicrobial agent from the group of fluoroquinolones. It has a bactericidal effect by inhibiting DNA gyrase, which provides supercoiling and stability of bacterial DNA, and leads to destabilization of the DNA chain and bacterial death.

Norfloxacin is susceptible in vivo to:

gram – positive aerobes – Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae; gram-negative aerobes-Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia E. coli, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens.

The following gram – negative aerobes are sensitive to norfloxacin in vitro:

Citrobacter diversus, Edwardsiella tarda, Enterobacter agglomerans, Haemophilus ducreyi, Klebsiella oxytoca, Morganella morganii, Providencia alcalifaciens, Providencia rettgeri, Providencia stuartii, Pseudomonas fluorescens, Pseudomonas stutzeri;

others – Ureaplasma urealyticum.

The drug is inactive against obligate anaerobes.

Pharmacokinetics:

Absorption by mouth is rapid (30-40%), food reduces absorption. The maximum concentration of norfloxacin in blood plasma (Cmax) when taking 200 mg,400 mg and 800 mg is 0.8 mcg / ml,1.5 mcg / ml and 2.4 mcg/ml, respectively. The time to reach the maximum concentration in blood plasma (TCmax) is 1 h. The effective half – life (T1/2) is 3-4 h. The equilibrium concentration of the drug in blood plasma (Css) is reached within 2 days.

Older excretion is slowed down (due to age-related decline in renal function): after intake of 400 mg norfloxacin area under the curve of concentration of a substance depending on the time parameters (AUC) is 6,97-12,63 mg*h/ml and Cmax – 1,25-of 2.79 µg/ml (young and 6.4 mg*h/ml and 1.5 µg/ml, respectively), T1/2 to 4 hours

Binding to plasma proteins is 10-15%.

In chronic renal failure (CRF) (creatinine clearance less than 30 ml/min/1.73 sq. m), T1 / 2 is extended to 6.5 hours.

Norfloxacin is metabolized in the liver. Renal clearance is 275 ml/min. Within 24 hours,26-32% is excreted by the kidneys in the form of unchanged substance,5-8% – in the form of a weakly active metabolite. Subsequently, less than 1% of the dose is excreted by the kidneys. About 30% is excreted by the intestines. In the elderly,22% of norfloxacin is excreted by the kidneys (renal clearance-154 ml / min).

2-3 hours after taking 400 mg orally, the concentration in the urine exceeds 200 mcg / ml, and for 12 hours it is maintained above 30 mcg / ml. At pH 7.5, the solubility of norfloxacin decreases.

Indications

Infections caused by microorganisms sensitive to norfloxacin: urinary tract infections (except acute and chronic complicated pyelonephritis), prostatitis, uncomplicated gonorrhea.

Use during pregnancy and lactation

The drug is contraindicated for use in pregnant women and women during lactation.

When used during lactation, breast-feeding should be discontinued.

Contraindications

Hypersensitivity; tendinitis, tendon rupture caused by taking fluoroquinolones (including in the anamnesis); pregnancy, lactation, childhood, glucose-6-phosphate dehydrogenase deficiency.

Use the drug with caution in the following diseases: :

Epilepsy, convulsive syndrome, renal / hepatic insufficiency, myasthenia gravis.

During the treatment period, patients should receive a sufficient amount of fluid (under the control of diuresis).

During therapy, an increase in the prothrombin index is possible (during surgical interventions, the state of the blood coagulation system should be monitored).

During treatment, avoid exposure to direct sunlight.

Norfloxacin, like other fluoroquinolones, can cause tendinitis and tendon rupture. Risk factors: age over 60 years, taking glucocorticosteroids, kidney, heart or lung transplantation, increased physical activity, CRF, a history of tendon damage (including rheumatoid arthritis). These phenomena may occur several months after the end of taking the drug. At the first sign of tendinitis or tendon rupture, you should stop taking norfloxacin and consult a doctor.

Norfloxacin can lower the threshold of convulsive readiness and cause seizures; fluoroquinolones can also stimulate the central nervous system, causing tremors, toxic psychoses, anxiety, confusion and hallucinations; increased intracranial pressure.

Norfloxacin can lead to the development of pseudomembranous colitis caused by Clostridium difficile. In this case, it is necessary to cancel the drug and prescribe appropriate treatment (the use of vancomycin inside or metronidazole).

Not effective for syphilis.

Norfloxacin may cause peripheral neuropathy (paresthesia, hypesthesia, dysesthesia, muscle weakness). At the first sign of neuropathy (pain, tingling, numbness or weakness in the extremities, violation of other types of sensitivity), the drug should be discontinued in order to avoid irreversible changes.

To avoid the formation of crystals of norfloxacin in the kidneys, do not exceed the recommended doses; it is necessary to take tablets with a sufficient amount of liquid.

Side effects

From the central nervous system (CNS): dizziness, headache, tingling in the fingers, drowsiness, anxiety, depression, insomnia, sleep disorders.

From the digestive system: nausea, abdominal pain, anorexia, diarrhea, pain in the rectum or anus, constipation, dyspepsia, flatulence, vomiting, dry oral mucosa, heartburn, loose stools, bitter taste in the mouth, ulceration of the oral mucosa, itching of the anus.

Hematopoietic disorders: leukopenia, thrombocytopenia, eosinophilia, neutropenia.

From the skin: pruritus, rash, erythema, urticaria.

From the side of the senses: blurred visual perception.

Musculoskeletal system disorders: bursitis, swelling of the hands and feet.

From the cardiovascular system (CVS): myocardial infarction, palpitation sensation.

From the urinary system: renal colic.

Laboratory parameters: increased activity of AST, ALT, ALP, LDH, proteinuria, decreased hematocrit and Hb, increased blood urea concentration, hypercreatininemia, glucosuria.

Other: hyperhidrosis, asthenia, back pain, fever, chills, chest pain, dysmenorrhea, edema, allergic reactions.

Post-marketing experience.

From the central nervous system: convulsions, myoclonia, tremor, peripheral neuropathy, Guillain-Barre syndrome, ataxia, paresthesia, hypesthesia, mental disorders (including confusion).

Allergic reactions: anaphylactoid reactions, angioedema, shortness of breath, vasculitis, arthritis, arthralgia, myalgia.

From the side of the skin: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, photosensitization.

From the digestive system: pseudomembranous colitis, hepatitis, cholestatic jaundice, pancreatitis, stomatitis, liver failure (including with a fatal outcome).

From the cardiovascular system: prolongation of the QT interval, ventricular arrhythmia, including tachycardia of the “pirouette” type.

From the urinary system: interstitial nephritis, renal failure.

Musculoskeletal disorders: tendinitis, tendon rupture, exacerbation of myasthenia gravis, increased CPK activity.

Hematopoietic disorders: agranulocytosis, hemolytic anemia.

Sensory disorders: hearing loss, tinnitus, diplopia, dysgeusia.

Other side effects when taking quinolones: albuminuria, candiduria, crystalluria, cylindruria, dysphagia, hyperglycemia, hypercholesterolemia, hyperkalemia, hypertriglyceridemia, hematuria, liver necrosis, hypoglycemia, nystagmus, postural hypotension, PV elongation, vaginal candidiasis.

Interaction

Reduces the clearance of theophylline by 25%, so when used simultaneously, the dose of theophylline should be reduced.

Increases the concentration of indirect anticoagulants, cyclosporine in the blood serum.

Reduces the effectiveness of nitrofurans.

Simultaneous administration of antacids containing aluminum or magnesium hydroxide, as well as drugs containing Fe, Zn2+, sucralfate, reduces the absorption of norfloxacin (the interval between their appointment should be at least 4 hours).

Concomitant use with drugs that reduce the threshold of convulsive readiness (including nonsteroidal anti-inflammatory drugs) may lead to the development of convulsions.

Norfloxacin in vitro inhibits the CYP1A2 isoenzyme, which can lead to an increase in the concentration of its substrates in the blood (including caffeine, clozapine, ropinirole, tacrin, theophylline, tizanidine).

When taken concomitantly with glibenclamide, severe hypoglycemia may develop.

Probenecid may reduce norfloxacin excretion.

Antacids, sucralfate, multivitamins containing zinc, didanosine should be taken 2 hours before or 2 hours after taking norfloxacin (may reduce its absorption).

How to take, course of use and dosage

Inside. For urinary tract infections-400 mg 2 times a day for 7-10 days; for uncomplicated cystitis-3-7 days; for chronic recurrent urinary tract infection-up to 12 weeks.

For acute bacterial gastroenteritis – 5 days.

In acute gonococcal urethritis, pharyngitis, proctitis, cervicitis – once 800 mg.

For typhoid fever – 400 mg 3 times a day for 14 days.

For the prevention of sepsis – 400 mg 2 times a day.

For the prevention of bacterial gastroenteritis-400 mg/day.

For the prevention of travelers ‘ diarrhea-400 mg / day 1 day before departure and during the entire travel period (no more than 21 days).

For the prevention of recurrent urinary tract infections-200 mg/day.

In patients with impaired renal function with creatinine clearance greater than 20 ml/min, no dosage adjustment is required. If creatinine clearance is less than 20 ml / min (or serum creatinine concentration is more than 5 mg / 100 ml) and patients on hemodialysis are prescribed 1/2 therapeutic dose 2 times a day or the full dose 1 time a day.

Overdose

Symptoms of overdose: dizziness, nausea, vomiting, drowsiness, “cold” sweat, puffy face without changes in the main hemodynamic parameters.

Treatment: gastric lavage, adequate hydration therapy with forced diuresis. It requires examination and observation in a hospital for several days.

There is no specific antidote.

Special instructions

Use the drug with caution in the following diseases:

Epilepsy, convulsive syndrome, renal / hepatic insufficiency, myasthenia gravis.

During the treatment period, patients should receive a sufficient amount of fluid (under the control of diuresis).

During therapy, an increase in the prothrombin index is possible (during surgical interventions, the state of the blood coagulation system should be monitored).

During treatment, avoid exposure to direct sunlight.

Norfloxacin, like other fluoroquinolones, can cause tendinitis and tendon rupture. Risk factors: age over 60 years, taking glucocorticosteroids, kidney, heart or lung transplantation, increased physical activity, CRF, a history of tendon damage (including rheumatoid arthritis). These phenomena may occur several months after the end of taking the drug. At the first sign of tendinitis or tendon rupture, you should stop taking norfloxacin and consult a doctor.

Norfloxacin can lower the threshold of convulsive readiness and cause seizures; fluoroquinolones can also stimulate the central nervous system, causing tremors, toxic psychoses, anxiety, confusion and hallucinations; increased intracranial pressure.

Norfloxacin can lead to the development of pseudomembranous colitis caused by Clostridium difficile. In this case, it is necessary to cancel the drug and prescribe appropriate treatment (the use of vancomycin inside or metronidazole).

Not effective for syphilis.

Norfloxacin may cause peripheral neuropathy (paresthesia, hypesthesia, dysesthesia, muscle weakness). At the first sign of neuropathy (pain, tingling, numbness or weakness in the extremities, violation of other types of sensitivity), the drug should be discontinued in order to avoid irreversible changes.

To avoid the formation of crystals of norfloxacin in the kidneys, do not exceed the recommended doses; it is necessary to take tablets with a sufficient amount of liquid.

Form of production

Tablets covered with a yellow film-coated color, biconvex, oblong shape with rounded ends, with a risk on one side.

The cross-section shows two layers, the inner layer is white or pale yellow.  

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Norfloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Urethritis, Prostatitis, Urinary Tract Infections, Diarrhea, Enteritis